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Terfenadine (Seldane) is a potent and selective histamine H1 receptor antagonist in asthmatic airways.
Am Rev Respir Dis 1987; 135(1):181-4AR

Abstract

Terfenadine (Seldane) is a new, highly potent H1 histamine receptor antagonist that in clinically effective doses is free of side effects. Because the low potency and specificity of many H1 receptor antagonists have made it difficult to define the precise role of histamine as a bronchoconstrictor mediator in asthma we have used terfenadine to define the degree and selectivity of H1 blockade that can be achieved in asthmatic airways. In a double-blind study, 9 asthmatic patients received placebo or terfenadine 60, 120, and 180 mg on separate days followed 3 h later by bronchial provocation with increasing concentrations of either histamine or methacholine. Terfenadine at 60, 120, and 180 mg produced significant bronchodilation with increases in FEV1 above baseline of 9.0, 9.5, and 10%, respectively (p less than 0.05, p less than 0.01, p less than 0.01). All 3 doses of terfenadine displaced the histamine-FEV1 concentration response curves in a parallel fashion to the right in all subjects. When the degree of protection against histamine is expressed as a concentration ratio, terfenadine 60, 120, and 180 mg displaced the response curves by factors of 14.8 +/- 4.6, 22.9 +/- 6.7, and 34.3 +/- 8.4. In contrast to its effect on histamine-induced bronchoconstriction, terfenadine failed to protect the airways against the constrictor effect of inhaled methacholine. Thus, terfenadine is a much more potent and selective H1 receptor antagonist in asthmatic airways than previously available antihistamines and should provide a powerful tool to define the contribution of histamine as a bronchoconstrictor mediator in asthma.

Authors

No affiliation info availableNo affiliation info available

Pub Type(s)

Clinical Trial
Comparative Study
Controlled Clinical Trial
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

2879489

Citation

Rafferty, P, and S T. Holgate. "Terfenadine (Seldane) Is a Potent and Selective Histamine H1 Receptor Antagonist in Asthmatic Airways." The American Review of Respiratory Disease, vol. 135, no. 1, 1987, pp. 181-4.
Rafferty P, Holgate ST. Terfenadine (Seldane) is a potent and selective histamine H1 receptor antagonist in asthmatic airways. Am Rev Respir Dis. 1987;135(1):181-4.
Rafferty, P., & Holgate, S. T. (1987). Terfenadine (Seldane) is a potent and selective histamine H1 receptor antagonist in asthmatic airways. The American Review of Respiratory Disease, 135(1), pp. 181-4.
Rafferty P, Holgate ST. Terfenadine (Seldane) Is a Potent and Selective Histamine H1 Receptor Antagonist in Asthmatic Airways. Am Rev Respir Dis. 1987;135(1):181-4. PubMed PMID: 2879489.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Terfenadine (Seldane) is a potent and selective histamine H1 receptor antagonist in asthmatic airways. AU - Rafferty,P, AU - Holgate,S T, PY - 1987/1/1/pubmed PY - 1987/1/1/medline PY - 1987/1/1/entrez SP - 181 EP - 4 JF - The American review of respiratory disease JO - Am. Rev. Respir. Dis. VL - 135 IS - 1 N2 - Terfenadine (Seldane) is a new, highly potent H1 histamine receptor antagonist that in clinically effective doses is free of side effects. Because the low potency and specificity of many H1 receptor antagonists have made it difficult to define the precise role of histamine as a bronchoconstrictor mediator in asthma we have used terfenadine to define the degree and selectivity of H1 blockade that can be achieved in asthmatic airways. In a double-blind study, 9 asthmatic patients received placebo or terfenadine 60, 120, and 180 mg on separate days followed 3 h later by bronchial provocation with increasing concentrations of either histamine or methacholine. Terfenadine at 60, 120, and 180 mg produced significant bronchodilation with increases in FEV1 above baseline of 9.0, 9.5, and 10%, respectively (p less than 0.05, p less than 0.01, p less than 0.01). All 3 doses of terfenadine displaced the histamine-FEV1 concentration response curves in a parallel fashion to the right in all subjects. When the degree of protection against histamine is expressed as a concentration ratio, terfenadine 60, 120, and 180 mg displaced the response curves by factors of 14.8 +/- 4.6, 22.9 +/- 6.7, and 34.3 +/- 8.4. In contrast to its effect on histamine-induced bronchoconstriction, terfenadine failed to protect the airways against the constrictor effect of inhaled methacholine. Thus, terfenadine is a much more potent and selective H1 receptor antagonist in asthmatic airways than previously available antihistamines and should provide a powerful tool to define the contribution of histamine as a bronchoconstrictor mediator in asthma. SN - 0003-0805 UR - https://www.unboundmedicine.com/medline/citation/2879489/Terfenadine__Seldane__is_a_potent_and_selective_histamine_H1_receptor_antagonist_in_asthmatic_airways_ L2 - http://www.atsjournals.org/doi/full/10.1164/arrd.1987.135.1.181?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -